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<p>The synthesis of (1<i>H-</i>1,2,3-triazol-4-yl)-1,2,4-triazolazine derivatives was achieved via a multi-step synthesis starting from 1<i>H-</i>1,2,3-triazole-4-carboxylic acids, followed by acylation and ring closure under the influence of POCl₃. The title compounds were tested for cytotoxicity against a range of cancer cell lines, including A549 human lung carcinoma, HCT116 colon carcinoma, Jurkat T-leukemia, and KB3-1 human cervical carcinoma. The compounds demonstrated varying degrees of activity, with several showing potent cytotoxic effects, particularly against human lung carcinoma A549 and human leukemia Jurkat T-cells. The results suggest that ring closure significantly influences the bioactivity of the compounds, enhancing their cytotoxic properties. The study indicates the potential of (1<i>H-</i>1,2,3-triazol-4-yl)-1,2,4-triazolazine derivatives as promising candidates for cancer therapy, especially those with specific substituent patterns that enhance their antiproliferative effects.</p><p></p>

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Design and synthesis of novel 1H-1,2,3-triazolecarbohydrazides and 1,2,4-triazoloazines based on them for anticancer drug discovery

  • 期刊论文

  • 发表日期：

    2025年5月2日

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  • Daria Zakopailo,
  • Yevhen Blashchak,
  • Mykola Тupychak,
  • Nataliya Finiuk,
  • Nazariy Pokhodylo

摘要

The synthesis of (1H-1,2,3-triazol-4-yl)-1,2,4-triazolazine derivatives was achieved via a multi-step synthesis starting from 1H-1,2,3-triazole-4-carboxylic acids, followed by acylation and ring closure under the influence of POCl₃. The title compounds were tested for cytotoxicity against a range of cancer cell lines, including A549 human lung carcinoma, HCT116 colon carcinoma, Jurkat T-leukemia, and KB3-1 human cervical carcinoma. The compounds demonstrated varying degrees of activity, with several showing potent cytotoxic effects, particularly against human lung carcinoma A549 and human leukemia Jurkat T-cells. The results suggest that ring closure significantly influences the bioactivity of the compounds, enhancing their cytotoxic properties. The study indicates the potential of (1H-1,2,3-triazol-4-yl)-1,2,4-triazolazine derivatives as promising candidates for cancer therapy, especially those with specific substituent patterns that enhance their antiproliferative effects.